Cited by 86HIV/AIDS drug development and treatmentHIV/AIDS Research and InterventionsNanoparticle-Based Drug Delivery

The DOI matches its Crossref record; 23 of the 23 references it cites were found in a registry or an index.

Formulation and pharmacology of long-acting rilpivirine

Williams, Peter E., Crauwels, Herta M., Basstanie, Esther D.·2015·Current Opinion in HIV and AIDS

Open this paper in CoChat — free account

Abstract

PURPOSE OF REVIEW: Rilpivirine (RPV), a nonnucleoside reverse transcriptase inhibitor, is a potent antiretroviral (ARV) effective for HIV treatment at 25 mg daily oral dose. Its physio-chemical and pharmacological properties enable formulation of RPV as a long-acting injectable nanosuspension. This review summarizes these properties supporting the potential of intermittent parenteral administration of rilpivirine long acting (RPV LA) in both treatment and prevention of HIV-1 infection. RECENT FINDINGS: RPV is unusual among ARVs in that its stability and solubility enable aqueous suspensions with high drug loading, so that injection volumes can be minimized. Such innovative nanosuspensions are well tolerated in animals and humans after intramuscular injection and provide sustained drug concentrations in systemic circulation. The pharmacological findings support further investigations of RPV LA injections every 4 or 8 weeks, both as a single agent for potential preexposure prophylaxis and as two-drug all-injectable maintenance therapy with cabotegravir long acting. SUMMARY: By building on expertise with long-acting injectable antipsychotic agents, RPV has been formulated as an agent for infrequent intramuscular dosing, in addition to its conventional oral tablet forms. The advantages of adherence to a regimen of intermittent injections may be significant.

Integrity signals

Registry

Crossref · 10.1097/coh.0000000000000164

Cites

23 of 23 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

This paper’s full text isn’t openly available, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Prevention of HIV-1 infection with early antiretroviral therapy.
Cohen, M. S., Chen, Y. Q., McCauley, M., Gamble, T., Hosseinipour, M. C., Kumarasamy, N., Hakim, J. G., Kumwenda, J., Grinsztejn, B., Pilotto, J. H. S., et al. (2011) · New England Journal of Medicine · doi:10.1056/nejmoa1105243 · Cited by 6,873
Preexposure chemoprophylaxis for HIV prevention in men who have sex with men.
Grant, R. M., Lama, J. R., Anderson, P. L., McMahan, V., Liu, A. Y., Vargas, L., Goicochea, P., Casapía, M., Guanira-Carranza, J. V., Ramirez-Cardich, M. E., et al. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa1011205 · Cited by 5,096
Antiretroviral prophylaxis for HIV prevention in heterosexual men and women.
Baeten, J. M., Donnell, D., Ndase, P., Mugo, N. R., Campbell, J. D., Wangisi, J., Tappero, J. W., Bukusi, E. A., Cohen, C. R., Katabira, E., et al. (2012) · New England Journal of Medicine · doi:10.1056/nejmoa1108524 · Cited by 3,256
In Search of a Novel Anti-HIV Drug: Multidisciplinary Coordination in the Discovery of 4-[[4-[[4-[(1 E )-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, Rilpivirine)
Janssen, P. A. J., Lewi, P. J., Arnold, E., Daeyaert, F. F. D., de Jonge, M. R., Heeres, J., Koymans, L. M. H., Vinkers, M. H., Guillemont, J., Pasquier, E., et al. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm040840e · Cited by 351
Self-citation
A Multicenter Randomized Controlled Trial of Nevirapine Versus a Combination of Zidovudine and Lamivudine to Reduce Intrapartum and Early Postpartum Mother‐to‐Child Transmission of Human Immunodeficiency Virus Type 1
Moodley, D., Moodley, J., Coovadia, H. M., Gray, G., McIntyre, J. A., Hofmyer, J., Nikodem, C., Hall, D. B., Gigliotti, M. C., Robinson, P. A., et al. (2003) · The Journal of Infectious Diseases · doi:10.1086/367898 · Cited by 345
TMC278, a Next-Generation Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI), Active against Wild-Type and NNRTI-Resistant HIV-1
Azijn, H., Tirry, I., Vingerhoets, J., de Béthune, M., Kraus, G., Boven, K., Jochmans, D., Craenenbroeck, E. V., Picchio, G., & Rimsky, L. T. (2009) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.00986-09 · Cited by 291
Long-acting injectable antiretrovirals for HIV treatment and prevention
Spreen, W. R., Margolis, D. A., & Pottage, J. C. (2013) · Current Opinion in HIV and AIDS · doi:10.1097/coh.0000000000000002 · Cited by 253
High-Dose Sertraline Strategy for Nonresponders to Acute Treatment for Obsessive-Compulsive Disorder
Ninan, P. T., Koran, L. M., Kiev, A., Davidson, J. R. T., Rasmussen, S. A., Zajecka, J., Robinson, D. G., Crits-Christoph, P. F., Mandel, F. S., & Austin, C. (2006) · The Journal of Clinical Psychiatry · doi:10.4088/jcp.v67n0103 · Cited by 246
Development of a long-acting injectable formulation with nanoparticles of rilpivirine (TMC278) for HIV treatment
Baert, L., Klooster, G. A. E. V. '., Dries, W., François, M., Wouters, A., Basstanie, E. D., Iterbeke, K., Stappers, F., Stevens, P., Schueller, L., et al. (2009) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2009.03.006 · Cited by 224
Self-citation
Assessment of Second-Line Antiretroviral Regimens for HIV Therapy in Africa
Paton, N. I., Kityo, C. M., Hoppé, A., Reid, A., Kambugu, A. D., Lugemwa, A., van Oosterhout, J. J., Kiconco, M., Siika, A. M., Mwebaze, R. M., et al. (2014) · New England Journal of Medicine · doi:10.1056/nejmoa1311274 · Cited by 203

Show all 23 references

Research works printed but not linked: 3

Whiteside, 2014, Morbid Mortal Week Rep, 5, 63
Fauci, 2014, ed, 370, 495
Casado, 2014, AIDS Rev, 16, 172

Sorted by citations

Nanotechnology’s frontier in combatting infectious and inflammatory diseases: prevention and treatment
Huang, Y., Guo, X., Wu, Y., Chen, X., Feng, L., Xie, N., & Shen, G. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01745-z · Cited by 537
Nanotechnology approaches for global infectious diseases
Kirtane, A. R., Verma, M., Karandikar, P., Furin, J., Langer, R., & Traverso, G. (2021) · Nature Nanotechnology · doi:10.1038/s41565-021-00866-8 · Cited by 520
Long-acting intramuscular cabotegravir and rilpivirine in adults with HIV-1 infection (LATTE-2): 96-week results of a randomised, open-label, phase 2b, non-inferiority trial
Margolis, D. A., González‐García, J., Stellbrink, H.-J., Eron, J. J., Yazdanpanah, Y., Podzamczer, D., Lutz, T., Angel, J. B., Richmond, G. J., Clotet, B., et al. (2017) · The Lancet · doi:10.1016/s0140-6736(17)31917-7 · Cited by 506
Self-citation
Nanomedicine formulations for the delivery of antiviral drugs: a promising solution for the treatment of viral infections
Lembo, D., Donalisio, M., Civra, A., Argenziano, M., & Cavalli, R. (2017) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2017.1360863 · Cited by 179
Nanocrystals as a master key to deliver hydrophobic drugs via multiple administration routes
McGuckin, M. B., Wang, J., Ghanma, R., Qin, N., Palma, S. D., Donnelly, R. F., & Paredes, A. J. (2022) · Journal of Controlled Release · doi:10.1016/j.jconrel.2022.03.012 · Cited by 182
Strengths, weaknesses, opportunities and challenges for long acting injectable therapies: Insights for applications in HIV therapy
Owen, A., & Rannard, S. P. (2016) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2016.02.003 · Cited by 161
Design, formulation and evaluation of novel dissolving microarray patches containing a long-acting rilpivirine nanosuspension
Crudden, M. T. C. M., Larrañeta, E., Clark, A., Jarrahian, C., Rein‐Weston, A., Lachau‐Durand, S., Niemeijer, N., Williams, P., Haeck, C. M., McCarthy, H. O., et al. (2018) · Journal of Controlled Release · doi:10.1016/j.jconrel.2018.11.002 · Cited by 140
Self-citation
Long-acting antiretrovirals: a new era for the management and prevention of HIV infection
Thoueille, P., Choong, E., Cavassini, M. L., Buclin, T., & Decosterd, L. A. (2021) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dkab324 · Cited by 148
Long-Acting HIV Drugs for Treatment and Prevention
Gulick, R. M., & Flexner, C. W. (2018) · Annual Review of Medicine · doi:10.1146/annurev-med-041217-013717 · Cited by 119
Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment
Wang, Y., Clercq, E. D., & Li, G. (2019) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2019.1673367 · Cited by 107
Pre-exposure prophylaxis 2.0: new drugs and technologies in the pipeline
Coelho, L. E., Torres, T. S., Veloso, V. G., Landovitz, R. J., & Grinsztejn, B. G. J. (2019) · The Lancet HIV · doi:10.1016/s2352-3018(19)30238-3 · Cited by 101
Etravirine-loaded dissolving microneedle arrays for long-acting delivery
Rojekar, S. V., Vora, L. K., Tekko, I. A., Volpe‐Zanutto, F., McCarthy, H. O., Vavia, P. R., & Donnelly, R. F. (2021) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2021.04.024 · Cited by 100
Long-acting injectable atovaquone nanomedicines for malaria prophylaxis
Bakshi, R. P., Tatham, L. M., Savage, A. C., Tripathi, A. K., Mlambo, G., Ippolito, M. M., Nenortas, E., Rannard, S. P., Owen, A., & Shapiro, T. A. (2018) · Nature Communications · doi:10.1038/s41467-017-02603-z · Cited by 90
Long-acting rilpivirine as potential pre-exposure prophylaxis for HIV-1 prevention (the MWRI-01 study): an open-label, phase 1, compartmental, pharmacokinetic and pharmacodynamic assessment
McGowan, I., Dezzutti, C. S., Siegel, A., Engstrom, J. C., Nikiforov, A., Duffill, K., Shetler, C., Richardson‐Harman, N., Abebe, K. Z., Back, D. J., et al. (2016) · The Lancet HIV · doi:10.1016/s2352-3018(16)30113-8 · Cited by 82
Self-citation
Recent advances in long-acting nanoformulations for delivery of antiretroviral drugs
Surve, D. H., & Jindal, A. B. (2020) · Journal of Controlled Release · doi:10.1016/j.jconrel.2020.05.022 · Cited by 68
Efficacy, Safety, and Durability of Long-Acting Cabotegravir and Rilpivirine in Adults With Human Immunodeficiency Virus Type 1 Infection: 5-Year Results From the LATTE-2 Study
Smith, G. H. R., Henry, W. K., Podzamczer, D., Masiá, M. D. M., Bettacchi, C. J., Arastéh, K., Jaeger, H., Khuong-Josses, M.-A., Montes-Ramírez, M. L., Stellbrink, H., et al. (2021) · Open Forum Infectious Diseases · doi:10.1093/ofid/ofab439 · Cited by 64
Design, Formulation, and Evaluation of Novel Dissolving Microarray Patches Containing Rilpivirine for Intravaginal Delivery
Crudden, M. T. C. M., Larrañeta, E., Clark, A., Jarrahian, C., Rein‐Weston, A., Creelman, B. P., Moyo, Y., Lachau‐Durand, S., Niemeijer, N., Williams, P., et al. (2019) · Advanced Healthcare Materials · doi:10.1002/adhm.201801510 · Cited by 64
Self-citation
Long-Acting Antiretrovirals: Where Are We now?
Nyaku, A. N., Kelly, S. G., & Taiwo, B. (2017) · Current HIV/AIDS Reports · doi:10.1007/s11904-017-0353-0 · Cited by 59
Recent developments of nanotherapeutics for targeted and long-acting, combination HIV chemotherapy
Gao, Y., Kraft, J. C., Yu, D., & Ho, R. J. Y. (2018) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2018.04.014 · Cited by 60
Regulation of Staphylococcus aureus Virulence and Application of Nanotherapeutics to Eradicate S. aureus Infection
Arunachalam, K., Pandurangan, P., Shi, C., & Lagoa, R. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15020310 · Cited by 48
Long-acting formulations for the treatment of latent tuberculous infection: opportunities and challenges
Swindells, S., Siccardi, M., Barrett, S. E., Olsen, D. B., Grobler, J. A., Podany, A. T., Nuermberger, E. L., Kim, P., Barry, C. E., Owen, A., et al. (2018) · The International Journal of Tuberculosis and Lung Disease · doi:10.5588/ijtld.17.0486 · Cited by 48
Impact of Formulation Parameters on In Vitro Release from Long-Acting Injectable Suspensions
Bao, Q., Zou, Y., Wang, Y., Choi, S. H., & Burgess, D. J. (2021) · The AAPS Journal · doi:10.1208/s12248-021-00566-0 · Cited by 45
Historical Perspective of Clinical Nano and Microparticle Formulations for Delivery of Therapeutics
Batty, C. J., Bachelder, E. M., & Ainslie, K. M. (2021) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2021.04.002 · Cited by 46
Patient-reported tolerability and acceptability of cabotegravir + rilpivirine long-acting injections for the treatment of HIV-1 infection: 96-week results from the randomized LATTE-2 study
Murray, M. I., Pulido, F., Mills, A., Ramgopal, M. N., LeBlanc, R. P., Jaeger, H., Canon, V., Dorey, D., Griffith, S. K., Mrus, J. M., et al. (2019) · HIV Research & Clinical Practice · doi:10.1080/25787489.2019.1661696 · Cited by 43
Emerging reverse transcriptase inhibitors for HIV-1 infection
Mohammad, A., Pannek, S., & Fichtenbaum, C. J. (2018) · Expert Opinion on Emerging Drugs · doi:10.1080/14728214.2018.1474202 · Cited by 42
Branched copolymer-stabilised nanoemulsions as new candidate oral drug delivery systems
Hobson, J., Edwards, S. E., Slater, R. A., Martin, P., Owen, A., & Rannard, S. P. (2018) · RSC Advances · doi:10.1039/c8ra01944d · Cited by 39
Rilpivirine long-acting for the prevention and treatment of HIV infection
Ferretti, F., & Boffito, M. (2018) · Current Opinion in HIV and AIDS · doi:10.1097/coh.0000000000000474 · Cited by 40
The Promise of Long-Acting Antiretroviral Therapies: From Need to Manufacture
Gendelman, H. E., McMillan, J., Bade, A. N., Edagwa, B., & Kevadiya, B. D. (2019) · Trends in Microbiology · doi:10.1016/j.tim.2019.02.009 · Cited by 39
Activity of a Long-Acting Injectable Bedaquiline Formulation in a Paucibacillary Mouse Model of Latent Tuberculosis Infection
Kaushik, A., Ammerman, N. C., Tyagi, S. K., Saini, V., Vervoort, I., Lachau‐Durand, S., Nuermberger, E. L., & Andries, K. (2019) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.00007-19 · Cited by 39
Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase
Singh, K. D., Sarafianos, S. G., & Sönnerborg, A. B. (2019) · Pharmaceuticals · doi:10.3390/ph12020062 · Cited by 37
A long acting nanoformulated lamivudine ProTide
Smith, N. S., Bade, A. N., Soni, D., Gautam, N., Alnouti, Y., Herskovitz, J., Ibrahim, I. M., Wojtkiewicz, M. S., Shetty, B. L. D., McMillan, J., et al. (2019) · Biomaterials · doi:10.1016/j.biomaterials.2019.119476 · Cited by 35
Development and Evaluation of Dissolving Microarray Patches for Co-administered and Repeated Intradermal Delivery of Long-acting Rilpivirine and Cabotegravir Nanosuspensions for Paediatric HIV Antiretroviral Therapy
Moffatt, K., Tekko, I. A., Vora, L. K., Volpe‐Zanutto, F., Hutton, A. R. J., Mistilis, J. J., Jarrahian, C., Akhavein, N., Weber, A. D., McCarthy, H. O., et al. (2022) · Pharmaceutical Research · doi:10.1007/s11095-022-03408-6 · Cited by 35
Long acting systemic HIV pre-exposure prophylaxis: an examination of the field
Lykins, W. R., Luecke, E. H., Johengen, D., van der Straten, A., & Desai, T. A. (2017) · Drug Delivery and Translational Research · doi:10.1007/s13346-017-0391-6 · Cited by 33
Pharmacokinetics of Long-Acting Aqueous Nano-/Microsuspensions After Intramuscular Administration in Different Animal Species and Humans—a Review
Nguyen, V. T., Darville, N., & Vermeulen, A. (2022) · The AAPS Journal · doi:10.1208/s12248-022-00771-5 · Cited by 33
Pharmacokinetics and antiviral activity of cabotegravir and rilpivirine in cerebrospinal fluid following long-acting injectable administration in HIV-infected adults
Letendre, S. L., Mills, A., Hagins, D. P., Swindells, S., Felizarta, F., DeVente, J., Bettacchi, C. J., Lou, Y., Ford, S. L., Sutton, K., et al. (2019) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dkz504 · Cited by 31
Self-citation
Optimizing the Preparation and Stability of Decorated Antiretroviral Drug Nanocrystals
Zhou, T., Lin, Z., Puligujja, P., Palandri, D. L., Hilaire, J. R., Araínga, M., Smith, N. S., Gautam, N., McMillan, J., Alnouti, Y., et al. (2018) · Nanomedicine · doi:10.2217/nnm-2017-0381 · Cited by 29
Creation of a long-acting rilpivirine prodrug nanoformulation
Hilaire, J. R., Bade, A. N., Sillman, B., Gautam, N., Herskovitz, J., Shetty, B. L. D., Wojtkiewicz, M. S., Szlachetka, A. M., Lamberty, B. G., Sravanam, S., et al. (2019) · Journal of Controlled Release · doi:10.1016/j.jconrel.2019.09.001 · Cited by 29
Population pharmacokinetics of the rilpivirine long-acting formulation after intramuscular dosing in healthy subjects and people living with HIV
Neyens, M., Crauwels, H. M., Ruixo, J. J. P., & Rossenu, S. (2021) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dkab338 · Cited by 27
Self-citation
Towards a Maraviroc long-acting injectable nanoformulation
Tatham, L. M., Savage, A. C., Dwyer, A. B., Siccardi, M., Scott, T., Vourvahis, M., Clark, A., Rannard, S. P., & Owen, A. (2018) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2018.04.009 · Cited by 27
Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Vanangamudi, M., Senthilkumar, P., Kathiravan, M. K., & Namasivayam, V. (2023) · Viruses · doi:10.3390/v15101992 · Cited by 26
Formulation of antiretroviral nanocrystals and development into a microneedle delivery system for potential treatment of HIV-associated neurocognitive disorder (HAND)
Abbate, M. T. A., Ramöller, I. K., Sabri, A. H. B., Paredes, A. J., Hutton, A. R. J., McKenna, P. E., Peng, K., Hollett, J. A., McCarthy, H. O., & Donnelly, R. F. (2023) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2023.123005 · Cited by 25
Long-Acting Cabotegravir for HIV/AIDS Prophylaxis
Engelman, K. D., & Engelman, A. (2021) · Biochemistry · doi:10.1021/acs.biochem.1c00157 · Cited by 22
Synthesis of a long acting nanoformulated emtricitabine ProTide
Soni, D., Bade, A. N., Gautam, N., Herskovitz, J., Ibrahim, I. M., Smith, N. A., Wojtkiewicz, M. S., Shetty, B. L. D., Alnouti, Y., McMillan, J., et al. (2019) · Biomaterials · doi:10.1016/j.biomaterials.2019.119441 · Cited by 21
HIV-1 Integrase Strand Transfer Inhibitors and Neurodevelopment
Foster, E. G., Gendelman, H. E., & Bade, A. N. (2022) · Pharmaceuticals · doi:10.3390/ph15121533 · Cited by 20
Layer by layer self-assembly for coating a nanosuspension to modify drug release and stability for oral delivery
Elbaz, N. M., Tatham, L. M., Owen, A., Rannard, S. P., & McDonald, T. O. (2023) · Food Hydrocolloids · doi:10.1016/j.foodhyd.2023.108908 · Cited by 19
Battle of the milky way: Lymphatic targeted drug delivery for pathogen eradication
Taheri, A., Bremmell, K. E., Joyce, P., & Prestidge, C. A. (2023) · Journal of Controlled Release · doi:10.1016/j.jconrel.2023.10.002 · Cited by 21
Controlled Solvent Removal from Antiviral Drugs and Excipients in Solution Enables the Formation of Novel Combination Multi-Drug-Motifs in Pharmaceutical Powders Composed of Lopinavir, Ritonavir and Tenofovir
Yu, J., Yu, D.-N., Lane, S., McConnachie, L. A., & Ho, R. J. Y. (2020) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2020.08.003 · Cited by 19
Discovery and Characterization of a Novel CD4-Binding Adnectin with Potent Anti-HIV Activity
Wensel, D. L., Sun, Y., Li, Z., Zhang, S., Picarillo, C., McDonagh, T., Fabrizio, D. A., Cockett, M. I., Krystal, M., & Davis, J. H. (2017) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.00508-17 · Cited by 18
Use of long-acting injectable antiretroviral agents for human immunodeficiency Virus: A review
Ariyo, O. E., & Jones, C. E. (2021) · Journal of Clinical Virology · doi:10.1016/j.jcv.2021.105032 · Cited by 18
Targeted drug delivery: designing nanocarriers for improved therapeutic action
Hussain, S., Arif, A., Mujeeb-ur-Rehman, & Shah, M. R. (2026) · Chemical Communications · doi:10.1039/d5cc07306e · Cited by 18
Synthesis and Characterization of Long-Acting Darunavir Prodrugs
Banoub, M. G., Bade, A. N., Lin, Z., Cobb, D. A., Gautam, N., Shetty, B. L. D., Wojtkiewicz, M. S., Alnouti, Y., McMillan, J., Gendelman, H. E., et al. (2019) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.9b00871 · Cited by 17
Clinical translation and envisioned impact of nanotech for infection control: Economy, government policy and public awareness
Ma, X., & Poma, A. (2024) · Elsevier eBooks · doi:10.1016/b978-0-12-823994-0.00004-9 · Cited by 15
Intracellular delivery of nano‐formulated antituberculosis drugs enhances bactericidal activity
Donnellan, S., Stone, V., Johnston, H. J., Giardiello, M., Owen, A., Rannard, S. P., Aljayyoussi, G., Swift, B. M. C., Tran, L., Watkins, C. A., et al. (2017) · Journal of Interdisciplinary Nanomedicine · doi:10.1002/jin2.27 · Cited by 14
Delivery of long-acting injectable antivirals
Hickey, M. B., Merisko-Liversidge, E. M., Remenar, J. F., & Namchuk, M. (2015) · Current Opinion in Infectious Diseases · doi:10.1097/qco.0000000000000214 · Cited by 13
Emerging Trends in the Long-Acting Antiretroviral Therapy: Current Status and Therapeutic Challenges
Labh, R., & Gupta, R. (2020) · Current HIV Research · doi:10.2174/1570162x18666200824104140 · Cited by 13
Innovative nanotechnology for infectious and inflammatory disease control: From diagnostics to therapeutics
Khosravi, F., Rahmani, P., & Jahanban‐Esfahlan, R. (2025) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2025.118551 · Cited by 13
Antiretroviral agents in pre-exposure prophylaxis: emerging and advanced trends in HIV prevention
Yap, P. K., Xin, G. L. L., Tan, Y. Y., Chellian, J., Gupta, G., Liew, Y. K., Collet, T., Dua, K., & Chellappan, D. K. (2019) · Journal of Pharmacy and Pharmacology · doi:10.1111/jphp.13107 · Cited by 13
Chemically Nano-Engineered Theranostics for Phytoconstituents as Healthcare Application
Gilani, S. J., Beg, S., Kala, C., Nomani, M. S., Mahapatra, D. K., Imam, S. S., & Taleuzzaman, M. (2019) · Current Biochemical Engineering · doi:10.2174/2212711906666190723144111 · Cited by 12
A first-in-human study of the novel HIV-fusion inhibitor C34-PEG4-Chol
Quinn, K., Traboni, C., Penchala, S. D., Bouliotis, G., Doyle, N., Libri, V., Khoo, S., Ashby, D., Weber, J. N., Nicosia, A., et al. (2017) · Scientific Reports · doi:10.1038/s41598-017-09230-0 · Cited by 10
Cabotegravir and rilpivirine for the treatment of HIV
Rial‐Crestelo, D., Pinto-Martínez, A., & Pulido, F. (2020) · Expert Review of Anti-infective Therapy · doi:10.1080/14787210.2020.1736561 · Cited by 10
Tuning the release rate of rilpivirine from PLGA-based in situ forming implants
Ulianova, Y. V., Ermolenko, Y. V., Tkachenko, S., Trukhan, V., Морозов, А. Н., & Gelperina, S. E. (2022) · Polymer Bulletin · doi:10.1007/s00289-022-04623-2 · Cited by 8
Current status of the small molecule anti-HIV drugs in the pipeline or recently approved
Umumararungu, T., Nyandwi, J. B., Katandula, J., Twizeyimana, E. F., Tomani, J. C. D., Gahamanyi, N., Ishimwe, N., Olawode, E. O., Habarurema, G., Mpenda, M., et al. (2024) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2024.117860 · Cited by 9
A Therapeutic Perspective of Living with Human Immunodeficiency Virus/AIDS in 2017
Cluck, D. B., & Underwood, R. F. (2017) · Nursing Clinics of North America · doi:10.1016/j.cnur.2017.10.009 · Cited by 8
Application of Nanotechnology in the Treatment of Infectious Diseases: An Overview
Mba, I. E., & Nweze, E. I. (2022) · Springer eBooks · doi:10.1007/978-981-16-9190-4_2 · Cited by 9
Bionanotechnology and bioMEMS (BNM): state-of-the-art applications, opportunities, and challenges
Borenstein, J. T., Cummins, G., Dutta, A., Hamad, E. M., Hughes, M. P., Jiang, X., Lee, H., Lei, K. F., Tang, X. S., Zheng, Y., et al. (2023) · Lab on a Chip · doi:10.1039/d3lc00296a · Cited by 9
Recent Advances in Nanoparticle-Based Antiretroviral Drug Delivery Systems for HIV Treatment and Prevention: A Comprehensive Review
Das, G., Shin, H., & Patra, J. K. (2025) · International Journal of Nanomedicine · doi:10.2147/ijn.s540578 · Cited by 6
Long-acting dolutegravir formulations prevent neurodevelopmental impairments in a mouse model
Foster, E. G., Sillman, B., Liu, Y., Summerlin, M., Kumar, V. S., Sajja, B. R., Cassidy, A. R., Edagwa, B., Gendelman, H. E., & Bade, A. N. (2023) · Frontiers in Pharmacology · doi:10.3389/fphar.2023.1294579 · Cited by 7
Rilpivirine, emtricitabine and tenofovir alafenamide: single-tablet combination for the treatment of HIV-1 infection in selected patients
Ogbuagu, O. E. (2016) · Expert Review of Anti-infective Therapy · doi:10.1080/14787210.2016.1255551 · Cited by 7
The future of pre-exposure prophylaxis (PrEP) for human immunodeficiency virus (HIV) infection
Özdener-Poyraz, A. E., Park, T. E., Kalabalik, J., & Gupta, R. (2017) · Expert Review of Anti-infective Therapy · doi:10.1080/14787210.2017.1309292 · Cited by 6
History: Potential, Challenges, and Future Development in Nanopharmaceutical Research and Industry
Ariën, A., & Stoffels, P. (2016) · Wiley eBooks · doi:10.1002/9783527800681.ch1 · Cited by 6
Efficacy and Safety of Cabotegravir–Rilpivirine in PLWH: A Real-World Study
Conti, G. N., Spampinato, S., VITO, A. D., Marıno, A., Cirelli, T., Coco, V., Mirabile, A., del Vecchio, R. F., Franco, A., Montineri, A., et al. (2025) · Viruses · doi:10.3390/v17111417 · Cited by 5
Long-Term Efficacy, Safety, and Durability of Cabotegravir and Rilpivirine as 2-Drug Oral Maintenance Therapy After 6 Years of Study
Sutton, K., Vente, J. D., LeBlanc, R. P., DeJesus, E., Smith, G. H. R., Mills, A., Baril, J.-G., Clair, M. S., Stancil, B. S., Vandermeulen, K., et al. (2022) · Open Forum Infectious Diseases · doi:10.1093/ofid/ofac067 · Cited by 5
Preclinical development and pharmacokinetic assessment in macaques of a multipurpose long-acting injectable suspension containing medroxyprogesterone acetate for contraception and rilpivirine for HIV prevention
Haeck, C. M., Boyd, P., Dimant, N., Barrail‐Tran, A., Gouget, H., Grand, R. L., Desjardins, D., & Malcolm, K. R. (2023) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2023.104590 · Cited by 4
Biotechnological Approaches in Infectious Diseases
Banerjee, S., Bose, S., Shukla, A. C., & Baig, M. R. (2024) · Interdisciplinary biotechnological advances · doi:10.1007/978-981-97-1148-2_15 · Cited by 3
Human immunodeficiency virus infection challenges: Current therapeutic limitations and strategies for improved management through long‐acting injectable formulation
Tanushree, T., Sharma, A., Monika, Singh, R. P., & Jhawat, V. (2024) · Reviews in Medical Virology · doi:10.1002/rmv.2563 · Cited by 3
Biologic Injections with Prolonged Action: Transforming Immune System Therapies
Murphy, L., Kelly, A., & O'Brien, S. (2024) · Annals of Pharmacy Practice and Pharmacotherapy · doi:10.51847/pdfiq5uouj · Cited by 3
In vivo behaviors of meloxicam nanocrystals by intravenous administration are not significantly affected by stabilizers
Ma, L., Li, Z., Ye, G., Li, M., Sui, X., Liu, B., Tian, B., Liu, Y., & Fu, Q. (2023) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2023.104380 · Cited by 2
A Concise Review of Existing Therapies and Recent Advances in the Management of HIV Infection
Lal, H., Kumar, T. P., Dutta, S., & Ram, K. (2020) · International Journal of Pharmaceutical Sciences Review and Research · doi:10.47583/ijpsrr.2020.v64i01.028 · Cited by 2
Long-acting injectable biologics: a game-changer in immunopharmacology
Jawad, A. A., Abdulkhaleq, Z. M., Oraibi, A. I., Abdalrahman, M. A., Abed, H. N., Aziz, H. A., Sagban, S., Al-bahrani, D. M., Altimari, U. S., Jawad, M. A., et al. (2025) · Pharmacia · doi:10.3897/pharmacia.72.e154045 · Cited by 1
Clinical Applications of Long Acting Injectables: Systemic and Local Drug Delivery
Witika, B. A., Poka, M., Makoni, P. A., Ramazani, F., & Nkanga, C. I. (2025) · Springer eBooks · doi:10.1007/978-3-031-72302-5_7 · Cited by 1
Solid Drug Nanoparticles
Unsworth, C., Savage, A. C., & Rannard, S. P. (2024) · Springer eBooks · doi:10.1007/978-3-031-59478-6_4 · Cited by 1
Long-acting drug delivery systems: applications for sexual and reproductive health
Galal, S., Jones, C., & Coward, K. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-821749-8.00013-6
Cerebrospinal fluid concentrations, viral suppression and biomarkers with long-acting cabotegravir and rilpivirine intramuscular injections
Yilmaz, A., Nicolò, A. D., D’Avolio, A., & Gisslén, M. (2025) · Antiviral Research · doi:10.1016/j.antiviral.2025.106243
Parenteral Administration of Drug Nanocrystals: The Role of Long-Acting Injectables
Sousa, C. C., Moreira, D. R. M., López-Vidal, L., & Paredes, A. J. (2026) · Springer eBooks · doi:10.1007/978-3-032-10238-6_5
BindingDB Entry 50022810: Current status of the small molecule anti-HIV drugs in the pipeline or recently approved.
BindingDB (2026) · UC San Diego · doi:10.7270/q22v2mzm

Authors: Williams, P. E., Crauwels, H. M., & Basstanie, E. D.
Affiliations: Janssen (Belgium) (BE)
Corresponding author: Williams, Peter E.
ORCID: Crauwels, Herta M.
Venue: Current Opinion in HIV and AIDS
Publisher: Ovid Technologies (Wolters Kluwer Health)
Published: 2015-07
Volume: 10
Issue: 4
Pages: 233-238
ISSN: 1746-630X (ISSN-L)
DOI: 10.1097/coh.0000000000000164
OpenAlex: W2395339327
Cited by: 86
References: 23
Citations by year: 2026: 3 · 2025: 6 · 2024: 7 · 2023: 9 · 2022: 8 · 2021: 10 · 2020: 5 · 2019: 14 · 2018: 10 · 2017: 9 · 2016: 4 · 2015: 1
FWCI: 6.22
Type: journal article
Language: en
Open access: closed
Locations: Current Opinion in HIV and AIDS (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Infectious Diseases › HIV/AIDS drug development and treatment
Health Sciences › Medicine › Infectious Diseases › HIV/AIDS Research and Interventions
Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords: rilpivirine, long-acting injectables, nanoparticle suspensions, HIV-1, non-nucleoside reverse transcriptase inhibitors, antiretroviral therapy, pre-exposure prophylaxis, cabotegravir, intramuscular injection, drug formulation, pharmacokinetics, drug solubility and stability
MeSH terms: Rilpivirine, Humans, HIV-1, HIV Infections, Reverse Transcriptase Inhibitors, Anti-HIV Agents

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Formulation and pharmacology of long-acting rilpivirine

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Citations

Cites

Cited by

Related

Metadata

Record

About these checks